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Selective Agonists and Antagonists of Formylpeptide Receptors: Duplex Flow Cytometry and Mixture-Based Positional Scanning Libraries [Articles] 9 Aug 2013 | 05:35 pm

The formylpeptide receptor (FPR1) and formylpeptide-like 1 receptor (FPR2) are G protein–coupled receptors that are linked to acute inflammatory responses, malignant glioma stem cell metastasis, and c...

Mechanisms of Transient Receptor Potential Vanilloid 1 Activation and Sensitization by Allyl Isothiocyanate [Articles] 9 Aug 2013 | 05:35 pm

Allyl isothiocyanate (AITC; aka, mustard oil) is a powerful irritant produced by Brassica plants as a defensive trait against herbivores and confers pungency to mustard and wasabi. AITC is widely used...

Extracellular Disulfide Bridges Serve Different Purposes in Two Homologous Chemokine Receptors, CCR1 and CCR5 [Articles] 9 Aug 2013 | 05:35 pm

In addition to the 7 transmembrane receptor (7TM)-conserved disulfide bridge between transmembrane (TM) helix 3 and extracellular loop (ECL)-2, chemokine receptors (CCR) contain a disulfide bridge bet...

Segregation of Family A G Protein-Coupled Receptor Protomers in the Plasma Membrane [Articles] 9 Aug 2013 | 05:35 pm

G protein–coupled receptors (GPCRs) transduce many important physiological signals and are targets for a large fraction of therapeutic drugs. Members of the largest family of GPCRs (family A) are thou...

Sox9b Is Required for Epicardium Formation and Plays a Role in TCDD-Induced Heart Malformation in Zebrafish [Articles] 9 Aug 2013 | 05:35 pm

Activation of the transcription factor aryl hydrocarbon receptor by 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD) prevents the formation of the epicardium and leads to severe heart malformations in devel...

Human Immunodeficiency Virus Protease Inhibitors Interact with ATP Binding Cassette Transporter 4/Multidrug Resistance Protein 4: A Basis for Unantici... 9 Aug 2013 | 05:35 pm

Human immunodeficiency virus (HIV) pharmacotherapy, by combining different drug classes such as nucleoside analogs and HIV protease inhibitors (PIs), has increased HIV-patient life expectancy. Consequ...

Connective Tissue Growth Factor/CCN2 Attenuates {beta}-Adrenergic Receptor Responsiveness and Cardiotoxicity by Induction of G Protein-Coupled Recepto... 9 Aug 2013 | 05:35 pm

Myocardial connective tissue growth factor (CTGF/CCN2) is induced in heart failure, a condition associated with diminution of β-adrenergic receptor (β-AR) responsiveness. Accordingly, we aimed to inve...

Novel Amino-Carbonitrile-Pyrazole Identified in a Small Molecule Screen Activates Wild-Type and {triangleup}F508 Cystic Fibrosis Transmembrane Conduct... 9 Aug 2013 | 05:35 pm

Cystic fibrosis (CF) is caused by loss-of-function mutations in the CF transmembrane conductance regulator (CFTR) Cl– channel. We developed a phenotype-based high-throughput screen to identify small-m...

{alpha}4{alpha}6{beta}2* Nicotinic Acetylcholine Receptor Activation on Ventral Tegmental Area Dopamine Neurons Is Sufficient to Stimulate a Depolariz... 9 Aug 2013 | 05:35 pm

Tobacco addiction is a serious threat to public health in the United States and abroad, and development of new therapeutic approaches is a major priority. Nicotine activates and/or desensitizes nicoti...

Potent Inhibition of Aldehyde Dehydrogenase-2 by Diphenyleneiodonium: Focus on Nitroglycerin Bioactivation [Articles] 9 Aug 2013 | 05:35 pm

Aldehyde dehydrogenase-2 (ALDH2) catalyzes vascular bioactivation of the antianginal drug nitroglycerin (GTN) to yield nitric oxide (NO) or a related species that activates soluble guanylate cyclase (...

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